A new EGFR inhibitor induces apoptosis in colon cancer cells

作者: N. Calonghi , E. Pagnotta , C. Parolin , C. Mangano , M.L. Bolognesi

DOI: 10.1016/J.BBRC.2006.12.214

关键词:

摘要: The use of agents targeting EGFR represents a new frontier in colon cancer therapy. Among these, mAbs and tyrosine kinase inhibitors seemed to be the most promising. However they have demonstrated scarce utility therapy, former being effective only at toxic doses, latter resulting inefficient cancer. This paper presents studies on inhibitor, FR18, molecule containing same naphtoquinone core as shikonin, an agent with great anti-tumor potential. In HT29, human carcinoma cell line, flow cytometry, immunoprecipitation, Western blot analysis, confocal spectral microscopy that FR18 is active concentrations low 10 nM, inhibits EGF binding while leaving unperturbed receptor activity. At concentration ranging from 30 nM 5 μM, it activates apoptosis. seems therefore possible therapeutic applications

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